Lead compounds discovered from libraries

被引：95
作者：
Golebiowski, A [1 ]
Klopfenstein, SR [1 ]
Portlock, DE [1 ]
机构：
[1] Procter & Gamble Pharmaceut, Hlth Care Res Ctr, Mason, OH 45040 USA
来源：
CURRENT OPINION IN CHEMICAL BIOLOGY | 2001年 / 5卷 / 03期
关键词：
D O I：
10.1016/S1367-5931(00)00203-9
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
Lead compounds with the potential to progress to viable drug candidates have been identified from libraries using several strategies. These include rapid screening of large diverse collections, thematic libraries, project-directed libraries, and three-dimensional molecular models of corporate databases. There have been numerous success stories, including the identification of several clinical candidates.
引用
收藏
页码：273 / 284
页数：12
相关论文
共 81 条
  • [1] 4-thiazolidinones: Novel inhibitors of the bacterial enzyme MurB
    Andres, CJ
    Bronson, JJ
    D'Andrea, SV
    Deshpande, MS
    Falk, PJ
    Grant-Young, KA
    Harte, WE
    Ho, HT
    Misco, PF
    Robertson, JG
    Stock, D
    Sun, YX
    Walsh, AW
    [J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2000, 10 (08) : 715 - 717
  • [2] Armstrong JI, 2000, ANGEW CHEM INT EDIT, V39, P1303, DOI 10.1002/(SICI)1521-3773(20000403)39:7<1303::AID-ANIE1303>3.0.CO
  • [3] 2-0
  • [4] Rational design of selective submicromolar inhibitors of Tritrichomonas foetus hypoxanthine-guanine-xanthine phosphoribosyltransferase
    Aronov, AM
    Munagala, NR
    de Montellano, PRO
    Kuntz, ID
    Wang, CC
    [J]. BIOCHEMISTRY, 2000, 39 (16) : 4684 - 4691
  • [5] A combinatorial approach toward the discovery of non-peptide, subtype-selective somatostatin receptor ligands
    Berk, SC
    Rohrer, SP
    Degrado, SJ
    Birzin, ET
    Mosley, RT
    Hutchins, SM
    Pasternak, A
    Schaeffer, JM
    Underwood, DJ
    Chapman, KT
    [J]. JOURNAL OF COMBINATORIAL CHEMISTRY, 1999, 1 (05): : 388 - 396
  • [6] Identification of a slow tight-binding inhibitor of 3-deoxy-D-manno-octulosonic acid 8-phosphate synthase
    Birck, MR
    Holler, TP
    Woodard, RW
    [J]. JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 2000, 122 (38) : 9334 - 9335
  • [7] Protein-based virtual screening of chemical databases. 1. Evaluation of different docking/scoring combinations
    Bissantz, C
    Folkers, G
    Rognan, D
    [J]. JOURNAL OF MEDICINAL CHEMISTRY, 2000, 43 (25) : 4759 - 4767
  • [8] Novel inhibitors of DNA gyrase: 3D structure based biased needle screening, hit validation by biophysical methods, and 3D guided optimization. A promising alternative to random screening
    Boehm, HJ
    Boehringer, M
    Bur, D
    Gmuender, H
    Huber, W
    Klaus, W
    Kostrewa, D
    Kuehne, H
    Luebbers, T
    Meunier-Keller, N
    [J]. JOURNAL OF MEDICINAL CHEMISTRY, 2000, 43 (14) : 2664 - 2674
  • [9] Total synthesis of distamycin A and 2640 analogues: A solution-phase combinatorial approach to the discovery of new, bioactive DNA binding agents and development of a rapid, high-throughput screen for determining relative DNA binding affinity or DNA binding sequence selectivity
    Boger, DL
    Fink, BE
    Hedrick, MP
    [J]. JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 2000, 122 (27) : 6382 - 6394
  • [10] Bohm H.J., 2000, VIRTUAL SCREENING BI
123456789